FULYZAQ

FULYZAQ- crofelemer tablet, coated
Napo Pharmaceuticals, Inc.

1 INDICATIONS AND USAGE

FULYZAQ is indicated for symptomatic relief of non-infectious diarrhea in patients with HIV/AIDS on anti-retroviral therapy.

2 DOSAGE AND ADMINISTRATION

The recommended dose of FULYZAQ is one 125 mg delayed-release tablet taken orally two times a day, with or without food. FULYZAQ tablets should not be crushed or chewed. Tablets should be swallowed whole.

3 DOSAGE FORMS AND STRENGTHS

FULYZAQ is a white, oval, enteric-coated 125 mg delayed-release tablet printed on one side with 125SLXP.

4 CONTRAINDICATIONS

None.

5 WARNINGS AND PRECAUTIONS

5. 1 Risks of Treatment in Patients with Infectious Diarrhea

If infectious etiologies are not considered, and FULYZAQ is initiated based on a presumptive diagnosis of non-infectious diarrhea, then there is a risk that patients with infectious etiologies will not receive the appropriate treatments, and their disease may worsen. Before starting FULYZAQ, rule out infectious etiologies of diarrhea. FULYZAQ is not indicated for the treatment of infectious diarrhea.

6 ADVERSE REACTIONS

6.1 Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. A total of 696 HIV-positive patients in three placebo-controlled trials received FULYZAQ for a mean duration of 78 days. Of the total population across the three trials, 229 patients received a dose of 125 mg twice a day for a mean duration of 141 days, 69 patients received a dose of 250 mg twice a day for a mean duration of 139 days, 102 patients received a dose of 250 mg four times a day for a mean duration of 14 days, 54 patients received a dose of 500 mg twice a day for a mean duration of 146 days, and 242 patients received a dose of 500 mg four times a day for a mean duration of 14 days.

Adverse reactions for FULYZAQ that occurred in at least 2% of patients and at a higher incidence than placebo are provided in Table 1.

Table 1: Adverse Reactions Occurring in at Least 2% of Patients in the 125 mg Twice Daily Group
Adverse Reaction Crofelemer 125 mg BID* N = 229 n (%) Placebo N = 274 n (%)
Upper respiratory tractinfection 13 (5.7) 4 (1.5)
Bronchitis 9 (3.9) 0
Cough 8 (3.5) 3 (1.1)
Flatulence 7 (3.1) 3 (1.1)
Increased bilirubin 7 (3.1) 3 (1.1)
Nausea 6 (2.6) 4 (1.5)
Back pain 6 (2.6) 4 (1.5)
Arthralgia 6 (2.6) 0
Urinary tract infection 5 (2.2) 2 (0.7)
Nasopharyngitis 5 (2.2) 2 (0.7)
Musculoskeletal pain 5 (2.2) 1 (0.4)
Hemorrhoids 5 (2.2) 0
Giardiasis 5 (2.2) 0
Anxiety 5 (2.2) 1 (0.4)
Increased alanine aminotransferase 5 (2.2) 3 (1.1)
Abdominal distension 5 (2.2) 1 (0.4)
* Twice daily

Adverse reactions that occurred in between 1% and 2% of patients taking a 250 mg daily dose of FULYZAQ were abdominal pain, acne, increased aspartate aminotransferase, increased conjugated bilirubin, increased unconjugated blood bilirubin, constipation, depression, dermatitis, dizziness, dry mouth, dyspepsia, gastroenteritis, herpes zoster, nephrolithiasis, pain in extremity, pollakiuria, procedural pain, seasonal allergy, sinusitis and decreased white blood cell count.

Adverse reactions were similar in patients who received doses greater than 250 mg daily.

7 DRUG INTERACTIONS

7.1 Drug Interaction Potential

In vitro studies have shown that crofelemer has the potential to inhibit cytochrome P450 isoenzyme 3A and transporters MRP2 and OATP1A2 at concentrations expected in the gut. Due to the minimal absorption of crofelemer, it is unlikely to inhibit cytochrome P450 isoenzymes 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 and CYP3A4 systemically [see Clinical Pharmacology (12.3)].

7.2 Nelfinavir, Zidovudine, and Lamivudine

FULYZAQ administration did not have a clinically relevant interaction with nelfinavir, zidovudine, or lamivudine in a drug-drug interaction trial.

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Pregnancy Category C

Reproduction studies performed with crofelemer in rats at oral doses up to 177 times the recommended daily human dose of 4.2 mg/kg revealed no evidence of impaired fertility or harm to the fetus. In pregnant rabbits, crofelemer at an oral dose of about 96 times the recommended daily human dose of 4.2 mg/kg, caused abortions and resorptions of fetuses. However, it is not clear whether these effects are related to the maternal toxicity observed. A pre- and postnatal development study performed with crofelemer in rats at oral doses of up to 177 times the recommended daily human dose of 4.2 mg/kg revealed no evidence of adverse pre- and postnatal effects in offspring. There are, however, no adequate, well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

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